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roxithromycin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibiotics, produced by Streptomyces strains | 2410 | 80214-83-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Semisynthetic derivative of erythromycin. It is concentrated by human phagocytes and is bioactive intracellularly. While the drug is active against a wide spectrum of pathogens, it is particularly effective in the treatment of respiratory and genital tract infections.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.30 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.19 mg/mL | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 12 % | Benet LZ, Broccatelli F, Oprea TI |
| BA (Bioavailability) | 50 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.401 | Moderate | 0.71 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 56.754 | Moderate | 0.71 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 1.294 | 10^-6 cm/s | Moderate | 0.71 |
| dh-clint | Dog hepatocyte intrinsic clearance | 6.353 | uL/min/10^6 cells | Moderate | 0.71 |
| dppb | Dog plasma protein binding (% unbound) | 51.320 | % | Moderate | 0.71 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 46.380 | % | Moderate | 0.71 |
| herg | hERG pIC50 | 4.207 | pIC50 | Moderate | 0.71 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.919 | uL/min/10^6 cells | Moderate | 0.71 |
| hlm-clint | Human liver microsomal intrinsic clearance | 22.909 | uL/min/mg protein | Moderate | 0.71 |
| hppb | Human plasma protein binding (% unbound) | 53.620 | % | Moderate | 0.71 |
| kinase-safety-class | ACVR2B,AXL,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAP3K21,MAPK7,NTRK2,PDK1,PDK2,PRKDC,TEK | 16 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 2.183 | Moderate | 0.78 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 7.691 | Moderate | 0.71 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 4.989 | Moderate | 0.71 | |
| mppb | Mouse plasma protein binding (% unbound) | 52.240 | Moderate | 0.71 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 8.356 | Moderate | 0.71 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | High | 1 | |
| pppb | Pig plasma protein binding (% unbound) | 64.480 | % | Moderate | 0.71 |
| rat-kpuu-brain | Rat brain Kpuu | 0.014 | % | Moderate | 0.78 |
| rh-clint | Rat hepatocyte intrinsic clearance | 4.121 | uL/min/10^6 cells | Moderate | 0.71 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 80.330 | % | Moderate | 0.71 |
| rppb | Rat plasma protein binding (% unbound) | 49.370 | % | Moderate | 0.71 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 862.979 | uM | Moderate | 0.71 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1987 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Varicella | 64.25 | 33.01 | 13 | 700 | 2052 | 42618570 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Varicella | 59.15 | 29.31 | 13 | 1488 | 3742 | 110584056 |
| Drug reaction with eosinophilia and systemic symptoms | 57.22 | 29.31 | 26 | 1475 | 82069 | 110505729 |
| Jaundice | 38.86 | 29.31 | 18 | 1483 | 59218 | 110528580 |
| Hepatitis fulminant | 30.29 | 29.31 | 9 | 1492 | 8551 | 110579247 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J01FA06 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE MACROLIDES, LINCOSAMIDES AND STREPTOGRAMINS Macrolides |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
Related Drugs by ATC class:
J01FA Macrolides 13 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.96 | acidic |
| pKa2 | 8.65 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Motilin receptor | GPCR | AGONIST | IC50 | 6.20 | IUPHAR | ||||
| 50S ribosomal protein L10 | Ribosomal protein | WOMBAT-PK | |||||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 6.26 | DRUG MATRIX |
External reference:
| ID | Source |
|---|---|
| N0000168422 | NUI |
| D01710 | KEGG_DRUG |
| C0035891 | UMLSCUI |
| CHEBI:32109 | CHEBI |
| ROX | PDB_CHEM_ID |
| CHEMBL1214185 | ChEMBL_ID |
| D015575 | MESH_DESCRIPTOR_UI |
| DB00778 | DRUGBANK_ID |
| 1465 | IUPHAR_LIGAND_ID |
| 5815 | INN_ID |
| 21KOF230FA | UNII |
| 6915744 | PUBCHEM_CID |
| 9478 | RXNORM |
| 004199 | NDDF |
| 713769006 | SNOMEDCT_US |
| 96037004 | SNOMEDCT_US |
Pharmaceutical products:
None